Identifying and developing new pharmaceuticals is a multibillion dollar industry in the U.S. alone. Gene specific transcription factors provide a promising class of targets for novel therapeutics directed to these and other human diseases. Urgently needed are efficient methods of identifying pharmacological agents or drugs which are active at the level of gene transcription. If amenable to automated, cost-effective, high throughput drug screening, such methods would have immediate application in a broad range of domestic and international pharmaceutical and biotechnology drug development programs.
Immunosuppression is therapeutically desirable in a wide variety of circumstances including transplantation, allergy and other forms of hypersensitivity, autoimmunity, etc. Cyclosporin, a widely used drug for effecting immunosuppression, is believed to act by inhibiting a calcineurin, a phosphatase which activates certain nuclear factors of activated T-cells (NFATs). However, because of side effects and toxicity, clinical indications of cyclosporin (and the more recently developed FK506) are limited.
Accordingly, it is desired to identify agents which more specifically interfere with the function of hNFATs. Unfortunately, the reagents necessary for the development of high-throughput screening assays for such therapeutics are unavailable.